SR33805 是钙通道拮抗剂,在去极化和极化条件下的EC50值分别为 4.1 和 33 nM。它阻止 L 型 Ca2+通道,可用于研究急性或慢性心脏衰竭。
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SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)
体外活性
Acute treatment with SR33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes.?Indeed, a SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation.?Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR33805.?Finally, administration of a single intra-peritoneal bolus of SR33805 (20 mg/kg) improved end-systolic strain and fractional shortening of MI hearts[1]
Cas No.
121345-64-0
分子式
C32H40N2O5S
分子量
564.74
别名
SR33805
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years